PE20060427A1 - Derivados de pirazol como inhibidores de la union del glucagon y composiciones - Google Patents

Derivados de pirazol como inhibidores de la union del glucagon y composiciones

Info

Publication number: PE20060427A1
Authority: PE; Peru
Prior art keywords: pirazole; derivatives; compositions; alkyl; binding inhibitors
Prior art date: 2004-06-04

Application number

PE2005000624A

Other languages

English (en)

Spanish (es)

Inventor

Emma R Parmee

Yusheng Xiong

Rui Liang

Linda Brockunier

Jian Guo

Original Assignee

Merck & Co Inc

Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)

2004-06-04

Filing date

2005-06-02

Publication date

2006-06-19

2005-06-02 Application filed by Merck & Co Inc filed Critical Merck & Co Inc

2006-06-19 Publication of PE20060427A1 publication Critical patent/PE20060427A1/es

Links

102000051325 Glucagon Human genes 0.000 title abstract 2
108060003199 Glucagon Proteins 0.000 title abstract 2
MASNOZXLGMXCHN-ZLPAWPGGSA-N glucagon Chemical compound C([C@@H](C(=O)N[C@H](C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(O)=O)C(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CO)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C1=CC=CC=C1 MASNOZXLGMXCHN-ZLPAWPGGSA-N 0.000 title abstract 2
229960004666 glucagon Drugs 0.000 title abstract 2
239000003112 inhibitor Substances 0.000 title abstract 2
239000000203 mixture Substances 0.000 title 1
229940000635 beta-alanine Drugs 0.000 abstract 2
150000001875 compounds Chemical class 0.000 abstract 2
WZKSXHQDXQKIQJ-UHFFFAOYSA-N F[C](F)F Chemical class F[C](F)F WZKSXHQDXQKIQJ-UHFFFAOYSA-N 0.000 abstract 1
CIUQDSCDWFSTQR-UHFFFAOYSA-N [C]1=CC=CC=C1 Chemical compound [C]1=CC=CC=C1 CIUQDSCDWFSTQR-UHFFFAOYSA-N 0.000 abstract 1
QUPDWYMUPZLYJZ-UHFFFAOYSA-N ethyl Chemical compound C[CH2] QUPDWYMUPZLYJZ-UHFFFAOYSA-N 0.000 abstract 1
239000008194 pharmaceutical composition Substances 0.000 abstract 1
208000001072 type 2 diabetes mellitus Diseases 0.000 abstract 1

Classifications

- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
- C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
- C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/415—1,2-Diazoles
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/18—Drugs for disorders of the alimentary tract or the digestive system for pancreatic disorders, e.g. pancreatic enzymes
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P27/00—Drugs for disorders of the senses
- A61P27/02—Ophthalmic agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/04—Anorexiants; Antiobesity agents
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
- A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond

Landscapes

Health & Medical Sciences (AREA)
Chemical & Material Sciences (AREA)
Organic Chemistry (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
General Health & Medical Sciences (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Public Health (AREA)
Veterinary Medicine (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
General Chemical & Material Sciences (AREA)
Chemical Kinetics & Catalysis (AREA)
Diabetes (AREA)
Hematology (AREA)
Obesity (AREA)
Biomedical Technology (AREA)
Neurosurgery (AREA)
Neurology (AREA)
Emergency Medicine (AREA)
Urology & Nephrology (AREA)
Endocrinology (AREA)
Cardiology (AREA)
Ophthalmology & Optometry (AREA)
Heart & Thoracic Surgery (AREA)
Vascular Medicine (AREA)
Child & Adolescent Psychology (AREA)
Hospice & Palliative Care (AREA)
Psychiatry (AREA)
Epidemiology (AREA)
Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Plural Heterocyclic Compounds (AREA)
Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
Nitrogen Condensed Heterocyclic Rings (AREA)

PE2005000624A 2004-06-04 2005-06-02 Derivados de pirazol como inhibidores de la union del glucagon y composiciones PE20060427A1 (es)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US57711604P	2004-06-04	2004-06-04

Publications (1)

Publication Number	Publication Date
PE20060427A1 true PE20060427A1 (es)	2006-06-19

Family

ID=35335786

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
PE2005000624A PE20060427A1 (es)	2004-06-04	2005-06-02	Derivados de pirazol como inhibidores de la union del glucagon y composiciones

Country Status (34)

Country	Link
US (2)	US7598285B2 (pt)
EP (1)	EP1756064B1 (pt)
JP (2)	JP4108739B2 (pt)
CN (1)	CN1964947A (pt)
AR (2)	AR049291A1 (pt)
AT (1)	ATE395338T1 (pt)
AU (2)	AU2005252183B2 (pt)
BR (1)	BRPI0511703B8 (pt)
CA (1)	CA2566945C (pt)
CR (1)	CR8766A (pt)
CY (1)	CY1108544T1 (pt)
DE (1)	DE602005006806D1 (pt)
DK (1)	DK1756064T3 (pt)
EA (1)	EA012431B1 (pt)
EC (1)	ECSP067062A (pt)
ES (1)	ES2306165T3 (pt)
GE (1)	GEP20094605B (pt)
HR (1)	HRP20080311T3 (pt)
IL (1)	IL179754A (pt)
MA (1)	MA28673B1 (pt)
MX (1)	MXPA06014084A (pt)
MY (1)	MY143599A (pt)
NI (1)	NI200600290A (pt)
NO (1)	NO339149B1 (pt)
NZ (1)	NZ551405A (pt)
PE (1)	PE20060427A1 (pt)
PL (1)	PL1756064T3 (pt)
PT (1)	PT1756064E (pt)
SI (1)	SI1756064T1 (pt)
TN (1)	TNSN06397A1 (pt)
TW (1)	TWI293952B (pt)
UA (1)	UA85884C2 (pt)
WO (1)	WO2005121097A2 (pt)
ZA (1)	ZA200609489B (pt)

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AR056574A1 (es) *	2005-10-19	2007-10-10	Merck & Co Inc	Derivados de pirazol, composiciones que contienen dichos compuestos y procedimientos de uso
WO2008087029A1 (en) *	2007-01-17	2008-07-24	Laboratorios Del Dr. Esteve, S.A.	Substituted pyrazoline compounds with acat inhibition activity
KR20160052792A (ko)	2007-02-09	2016-05-12	메타베이시스 테라퓨틱스, 인크.	글루카곤 수용체의 길항제
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US8232413B2 (en) *	2007-09-12	2012-07-31	Merck Sharp & Dohme Corp.	Process for the production of a crystalline glucagon receptor antagonist compound
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KR101569227B1 (ko)	2008-03-11	2015-11-13	아스카 세이야쿠 가부시키가이샤	고체 분산체와 그 의약 조성물, 그리고 그들의 제조 방법
CA2724294A1 (en)	2008-05-16	2009-11-19	Schering Corporation	Glucagon receptor antagonists, compositions, and methods for their use
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RU2008135294A (ru) *	2008-08-29	2010-03-10	Дик Корпорейшн (Jp)	Нафталиновые производные
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EP2350020B1 (en) *	2008-10-03	2014-08-13	Merck Sharp & Dohme Corp.	Spiro-imidazolone derivatives as glucagon receptor antagonists
US8324384B2 (en)	2009-02-12	2012-12-04	Merck Sharp & Dohme Corp.	Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
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EP2440553B1 (en) *	2009-06-12	2017-08-23	Merck Sharp & Dohme Corp.	Thiophenes as glucagon receptor antagonists, compositions, and methods for their use
EP2480077B1 (en)	2009-09-22	2015-02-18	Merck Sharp & Dohme Corp.	Pyrrolidines as glucagon receptor antagonists, compositions, and methods for their use
WO2012085745A1 (en)	2010-12-23	2012-06-28	Pfizer Inc.	Glucagon receptor modulators
EP2673260B1 (en)	2011-02-08	2016-08-17	Pfizer Inc	Glucagon receptor modulator
JP5647379B2 (ja)	2011-07-22	2014-12-24	ファイザー・インク	キノリニルグルカゴン受容体モジュレーター
TW201427658A (zh) *	2012-12-10	2014-07-16	Merck Sharp & Dohme	藉由投予升糖素受體拮抗劑及膽固醇吸收抑制劑治療糖尿病之方法
US9649294B2 (en)	2013-11-04	2017-05-16	Merck Sharp & Dohme Corp.	Glucagon receptor antagonist compounds, compositions containing such compounds and methods of use
CN103933032B (zh) *	2013-12-30	2019-08-23	北京赛林泰医药技术有限公司	作为抗癌药物的吡唑类衍生物的使用方法和用途
WO2015191900A1 (en)	2014-06-12	2015-12-17	Ligand Pharmaceuticals, Inc.	Glucagon antagonists
SG11201901355SA (en)	2016-08-30	2019-03-28	Regeneron Pharma	Methods of treating severe insulin resistance by interfering with glucagon receptor signaling
TWI763705B (zh) *	2016-09-06	2022-05-11	比利時商健生藥品公司	可作為升糖素受體拮抗劑之吲哚衍生物
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US6762318B2 (en)	2001-12-03	2004-07-13	Novo Nordisk A/S	Glucagon antagonists
WO2003051357A1 (en)	2001-12-19	2003-06-26	Novo Nordisk A/S	Glucagon receptor antagonists/inverse agonists
AU2002347022A1 (en)	2001-12-20	2003-07-09	Novo Nordisk A/S	Benzimidazols and indols as glucagon receptor antagonists/inverse agonisten
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EP1590336B1 (en)	2003-01-27	2010-12-01	Merck Sharp & Dohme Corp.	Substituted pyrazoles, compositions containing such compounds and methods of use
BRPI0409447A (pt) *	2003-04-14	2006-04-18	Inst For Pharm Discovery Inc	ácidos fenilalcanóicos substituìdos
AU2004238240A1 (en) *	2003-05-09	2004-11-25	Merck & Co., Inc.	Benzimidazoles, compositions containing such compounds and methods of use
DE602005006806D1 (de)	2004-06-04	2008-06-26	Merck & Co Inc	Pyrazolderivate, zusammensetzungen, die solche verbindungen enthalten, und anwendungsverfahren
DE602005021494D1 (de) *	2004-07-22	2010-07-08	Merck Sharp & Dohme	Substituierte pyrazole, derartige verbindungen enthaltende zusammensetzungen und verfahren zu ihrer verwendung
AR056574A1 (es) *	2005-10-19	2007-10-10	Merck & Co Inc	Derivados de pirazol, composiciones que contienen dichos compuestos y procedimientos de uso

2005
- 2005-05-31 DE DE602005006806T patent/DE602005006806D1/de not_active Expired - Lifetime
- 2005-05-31 CA CA2566945A patent/CA2566945C/en not_active Expired - Fee Related
- 2005-05-31 EP EP05754758A patent/EP1756064B1/en not_active Expired - Lifetime
- 2005-05-31 WO PCT/US2005/018828 patent/WO2005121097A2/en not_active Ceased
- 2005-05-31 MY MYPI20052470A patent/MY143599A/en unknown
- 2005-05-31 GE GEAP20059788A patent/GEP20094605B/en unknown
- 2005-05-31 CN CNA2005800182634A patent/CN1964947A/zh active Pending
- 2005-05-31 EA EA200602196A patent/EA012431B1/ru not_active IP Right Cessation
- 2005-05-31 ES ES05754758T patent/ES2306165T3/es not_active Expired - Lifetime
- 2005-05-31 AT AT05754758T patent/ATE395338T1/de active
- 2005-05-31 BR BRPI0511703A patent/BRPI0511703B8/pt not_active IP Right Cessation
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Also Published As

Publication number	Publication date
BRPI0511703A (pt)	2008-01-08
AU2008229701B2 (en)	2010-03-04
AR049291A1 (es)	2006-07-12
US7598285B2 (en)	2009-10-06
TNSN06397A1 (en)	2008-02-22
CR8766A (es)	2007-08-28
JP4108739B2 (ja)	2008-06-25
DE602005006806D1 (de)	2008-06-26
MA28673B1 (fr)	2007-06-01
BRPI0511703B8 (pt)	2021-05-25
CN1964947A (zh)	2007-05-16
AR088919A2 (es)	2014-07-16
UA85884C2 (uk)	2009-03-10
EP1756064A2 (en)	2007-02-28
US20090176854A1 (en)	2009-07-09
MXPA06014084A (es)	2007-02-15
NO339149B1 (no)	2016-11-14
EP1756064B1 (en)	2008-05-14
DK1756064T3 (da)	2008-09-22
MY143599A (en)	2011-06-15
NZ551405A (en)	2009-06-26
US7799818B2 (en)	2010-09-21
WO2005121097A2 (en)	2005-12-22
IL179754A (en)	2013-12-31
AU2005252183A1 (en)	2005-12-22
HRP20080311T3 (hr)	2008-07-31
AU2005252183B2 (en)	2008-07-17
CA2566945C (en)	2010-09-21
ZA200609489B (en)	2007-10-31
EA200602196A1 (ru)	2007-06-29
NO20070073L (no)	2007-03-05
EA012431B1 (ru)	2009-10-30
ES2306165T3 (es)	2008-11-01
JP2008150388A (ja)	2008-07-03
SI1756064T1 (sl)	2008-12-31
JP2008505062A (ja)	2008-02-21
BRPI0511703B1 (pt)	2018-07-17
TWI293952B (en)	2008-03-01
JP4733153B2 (ja)	2011-07-27
AU2008229701C1 (en)	2010-07-29
PL1756064T3 (pl)	2008-11-28
PT1756064E (pt)	2008-07-22
US20050272794A1 (en)	2005-12-08
CY1108544T1 (el)	2014-04-09
GEP20094605B (en)	2009-02-10
IL179754A0 (en)	2007-05-15
TW200604179A (en)	2006-02-01
AU2008229701A1 (en)	2008-10-30
WO2005121097A3 (en)	2006-02-16
NI200600290A (es)	2007-08-07
CA2566945A1 (en)	2005-12-22
ECSP067062A (es)	2007-01-26
ATE395338T1 (de)	2008-05-15

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Legal Events

Date	Code	Title	Description
2008-12-17	FG	Grant, registration
2019-01-30	FD	Application declared void or lapsed